[HTML][HTML] Targeted protein degradation: current molecular targets, localization, and strategies
D Pliatsika, C Blatter, R Riedl - Drug Discovery Today, 2024 - Elsevier
Targeted protein degradation (TPD) has revolutionized drug discovery by selectively
eliminating specific proteins within and outside the cellular context. Over the past two …
eliminating specific proteins within and outside the cellular context. Over the past two …
An updated patent review of BRD4 degraders
Introduction Bromodomain-containing protein 4 (BRD4), an important epigenetic reader, is
closely associated with the pathogenesis and development of many diseases, including …
closely associated with the pathogenesis and development of many diseases, including …
Heat Shock Protein 90 Interactome-Mediated Proteolysis Targeting Chimera (HIM-PROTAC) Degrading Glutathione Peroxidase 4 to Trigger Ferroptosis
J Dong, F Ma, M Cai, F Cao, H Li, H Liang… - Journal of Medicinal …, 2024 - ACS Publications
Targeted protein degradation (TPD) is an emerging therapeutic paradigm aimed at
eliminating the disease-causing protein with aberrant expression. Herein, we report a new …
eliminating the disease-causing protein with aberrant expression. Herein, we report a new …
Conformational diversity and protein–protein interfaces in drug repurposing in Ras signaling pathway
We focus on drug repurposing in the Ras signaling pathway, considering structural
similarities of protein–protein interfaces. The interfaces formed by physically interacting …
similarities of protein–protein interfaces. The interfaces formed by physically interacting …
Targeted Degradation of Protein Kinase A via a Stapled Peptide PROTAC
MK Whittaker, GN Bendzunas, M Shirani… - ACS Chemical …, 2024 - ACS Publications
Proteolysis-targeting chimeras (PROTACs) are bifunctional molecules that bind and recruit
an E3 ubiquitin ligase to a targeted protein of interest, often through the utilization of a small …
an E3 ubiquitin ligase to a targeted protein of interest, often through the utilization of a small …
Research progress of PROTACs for neurodegenerative diseases therapy
Neurodegenerative diseases (NDD) are characterized by the gradual deterioration of
neuronal function and integrity, resulting in an overall decline in brain function. The existing …
neuronal function and integrity, resulting in an overall decline in brain function. The existing …
New implications for prion diseases therapy and prophylaxis
F Liu, W Lü, L Liu - Frontiers in Molecular Neuroscience, 2024 - frontiersin.org
Prion diseases are rare, fatal, progressive neurodegenerative disorders that affect both
animal and human. Human prion diseases mainly present as Creutzfeldt-Jakob disease …
animal and human. Human prion diseases mainly present as Creutzfeldt-Jakob disease …
Targeting EGFR with molecular degraders as a promising strategy to overcome resistance to EGFR inhibitors
Q Wang, Y Zhu, J Pei - Future Medicinal Chemistry, 2024 - Taylor & Francis
Abnormal activation of EGFR is often associated with various malignant tumors, making it an
important target for antitumor therapy. However, traditional targeted inhibitors have several …
important target for antitumor therapy. However, traditional targeted inhibitors have several …
Molecular Glue-Mediated Targeted Protein Degradation: A Novel Strategy in Small-Molecule Drug Development
X Tan, Z Huang, H Pei, Z Jia, J Zheng - iScience, 2024 - cell.com
Small-molecule drugs are effective and thus most widely used. However, their applications
are limited by their reliance on active high-affinity binding sites, restricting their target …
are limited by their reliance on active high-affinity binding sites, restricting their target …
Inhibitors to degraders: Changing paradigm in drug discovery
V Haridas, S Dutta, A Munjal, S Singh - Iscience, 2024 - cell.com
The chemical understanding of biological processes provides not only a deeper insight but
also a solution to abnormal biological functioning. Protein degradation, a natural biological …
also a solution to abnormal biological functioning. Protein degradation, a natural biological …